Antiproliferative mechanisms of the flavonoids 2,2'-dihydroxychalcone and fisetin in human prostate cancer cells.

We have previously demonstrated the antiproliferative effect of two flavonoids-2,2'-dihydroxychalcone (DHC), a novel synthetic flavonoid, and fisetin, a naturally occurring flavonol-in prostate cancer cells. In this study, we further examine the mechanisms of these compounds on survival and prolifer...

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Published in:Nutrition & Cancer Vol. 62; no. 5; pp. 668 - 682
Main Authors: Haddad AQ, Fleshner N, Nelson C, Saour B, Musquera M, Venkateswaran V, Klotz L
Format: equations & formulas research tables/charts Journal Article
Published: Taylor & Francis Ltd Jul2010
Online Access:View this record in EBSCOhost
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      dt: Jul2010
      vid: 62
      iid: 5
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      pub: Taylor & Francis Ltd
      place: Philadelphia, Pennsylvania
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        atl: Antiproliferative mechanisms of the flavonoids 2,2'-dihydroxychalcone and fisetin in human prostate cancer cells.
      aug:
        au:
          Haddad AQ
          Fleshner N
          Nelson C
          Saour B
          Musquera M
          Venkateswaran V
          Klotz L
        affil: Sunnybrook Health Sciences Centre, Toronto, Ontario, Canada
      sug:
        subj:
          Cell Physiology
          Flavonoids Therapeutic Use
          Prostatic Neoplasms Physiopathology
          Apoptosis
          Biological Assay Methods
          Cell Cycle Physiology
          Funding Source
          Human
          Immunoblotting Methods
          Neoplasms
          Nutrition
          Polymerase Chain Reaction Methods
          Prostatic Neoplasms Mortality
          Proteins Physiology
          Survival
      ab: We have previously demonstrated the antiproliferative effect of two flavonoids-2,2'-dihydroxychalcone (DHC), a novel synthetic flavonoid, and fisetin, a naturally occurring flavonol-in prostate cancer cells. In this study, we further examine the mechanisms of these compounds on survival and proliferation pathways. DHC and fisetin (1-50 [mu]M) caused a dose-dependent reduction in viability, a concomitant increase in apoptosis in PC3 cells at 72 h, and a decrease in clonogenic survival at 24 h treatment. DHC was considerably more potent than fisetin in these cytotoxicity assays. The mechanism of accelerated cellular senescence was not activated by either compound in PC3 or lymph node carcinoma of the prostate (LNCaP) cells. Gene expression alterations in PC3 and LNCaP cells treated with 15 [mu]M DHC and 25 [mu]M fisetin for 6 to 24 h were determined by oligonucleotide array. Amongst the most highly represented functional categories of genes altered by both compounds was the cell cycle category. In total, 100 cell cycle genes were altered by DHC and fisetin including 27 genes with key functions in G2/M phase that were downregulated by both compounds. Other functional categories altered included chromosome organization, apoptosis, and stress response. These results demonstrate the multiple mechanisms of antitumor activity of DHC and fisetin in prostate cancer cells in vitro.
      pubtype: Academic Journal
      doctype:
        equations & formulas
        research
        tables/charts
        Journal Article
      ougenre: Article
    language: English
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